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Although the phase I clinical trial of LMB was unsuccessful
2019-11-04
Although the phase I clinical trial of LMB was unsuccessful, the detailed review of this trial only mentions some malaise and anorexia as side effects, which are common for most effective chemotherapeutic drugs. These side effects may diminish if lower doses are administered. In view of the novel CR
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br Conclusion br Introduction Biological wastewater treatmen
2019-11-04
Conclusion Introduction Biological wastewater treatment is targeted towards the removal of phosphorous, nitrogen and organic substances by the metabolic activity of a diverse activated sludge microbial community. More precisely, it is based on the versatile catalytic activity of the microbial
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We can think of two ways in
2019-11-04
We can think of two ways in which collagen binding could activate DDR (Figure 8). A single collagen triple helix could interact with both DS domains in the DDR dimer (“composite binding site”) and thereby activate the receptor, similar to the situation exemplified by the growth hormone-growth hormon
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br Discussion Previous studies have reported conflicting ass
2019-11-04
Discussion Previous studies have reported conflicting association results between the functional variant DBH −1021C>T and PD [8], [9]. Our findings would suggest that DBH −1021C>T does not dramatically decrease the risk of disease although it may marginally affect symptomatic AAO. However, whethe
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The results of bisaryl ether linker study are shown in
2019-11-04
The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th
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In summary we have identified a series of
2019-11-04
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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In the present study we investigated the role of EP
2019-11-04
In the present study, we investigated the role of EP1R after ICH and its mechanism of action. We hypothesized that EP1R activation aggravates ICH injury but that its blockade reduces injury through the Src kinases and the MMP-9 signaling pathway. To test this hypothesis, we examined the effects of s
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Methods br Results First we compared A plaque
2019-11-04
Methods Results First, we compared Aβ plaque number, Aβ concentration, and neurobehavior functions between naive APP/PS1 and APP/PS1xEP1−/− mice. Significantly lower Aβ burden in APP/PS1xEP1−/− mice was evidenced by fewer plaques in the hippocampal area and a lower concentration of soluble Aβ42
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For this reason downstream components of the inflammatory pa
2019-11-04
For this reason, downstream components of the inflammatory pathway have been investigated in the search for alternative targets. Targeting such downstream elements might result in safer and more tolerable analgesics. PGE mediates its effects through binding to four G-protein-coupled receptors (EP1-4
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VMD v Humphrey et al was
2019-11-04
VMD v1.9.2 (Humphrey et al., 1996) was used to analyze the MD trajectories, salt bridge interactions and secondary structure information from each frame. Once the model was optimized, the topological diagram and area and volume of protein cavities were analyzed using PDBsum (Laskowski, 2009) and CAS
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Protein ubiquitination occurs at the lysine residues and
2019-11-02
Protein ubiquitination occurs at the lysine residues, and is mediated by the sequential reactions of ubiquitin-activating enzyme (E1), conjugating enzyme (E2), and ligase (E3). The first step in this process comprises the ATP-dependent activation of ubiquitin by E1 to form a ubiquitin–E1 conjugate.
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Another enzyme class that has emerged as a potential alterna
2019-11-02
Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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br Conflict of interest br Acknowledgements This
2019-11-02
Conflict of interest Acknowledgements This work was supported by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP: 2014/00926-3). Introduction The metacestodes of Taenia solium are the causative agent of cysticercosis, which mainly resides the skeletal muscles and the central n
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br Conclusions Mulan is a mitochondrial E ubiquitin ligase w
2019-11-02
Conclusions Mulan is a mitochondrial E3 ubiquitin ligase with diverse roles in cell growth, cell death, and mitophagy. To better understand the mechanism of Mulan\'s function we used a modified yeast two-hybrid system to isolate proteins that interact with its cytoplasmic RING domain (amino acids
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Recent studies from the literature have
2019-11-02
Recent studies from the literature have identified new donepezil hydrochloride australia of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phen
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